HRP20240283T1 - Derivati 4-fluoro-1h-pirazolo[3,4-c]piridina kao selektivni inhibitori brutonove tirozin kinaze (btk) za liječenje b-staničnih limfoma i autoimunih bolesti - Google Patents

Derivati 4-fluoro-1h-pirazolo[3,4-c]piridina kao selektivni inhibitori brutonove tirozin kinaze (btk) za liječenje b-staničnih limfoma i autoimunih bolesti Download PDF

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HRP20240283T1
HRP20240283T1 HRP20240283TT HRP20240283T HRP20240283T1 HR P20240283 T1 HRP20240283 T1 HR P20240283T1 HR P20240283T T HRP20240283T T HR P20240283TT HR P20240283 T HRP20240283 T HR P20240283T HR P20240283 T1 HRP20240283 T1 HR P20240283T1
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Chunli SHEN
Xiawei WEI
Chengde Wu
Guoping Hu
Ning Jiang
Wei Zheng
Jian Li
Shuhui Chen
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Jumbo Drug Bank Co., Ltd.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (15)

1. Spoj prikazan kao formula (I), njegov stereoizomer ili njegova farmaceutski prihvatljiva sol, [image] pri čemu, T1 je neovisno izabran od N i CH; R2 je neovisno izabran od H, C1-6 alkila, C2-6 alkenila i C2-6 alkinila, pri čemu, svaki C1-6 alkil, C2-6 alkenil i C2-6 alkinil je neovisno i izborno supstituiran sa 1, 2 ili 3 Ra; prsten A je izabran od fenila i heteroarila sa 5 do 6 članova; M je neovisno izabran od C3-6 cikloalkila i heterocikloalkila sa 3 do 6 članova, pri čemu, svaki C3-6 cikloalkil i heterocikloalkil sa 3 do 6 članova je neovisno i izborno supstituiran sa 1, 2 ili 3 Rb; svaki R1 i R3 je neovisno izabran od F, Cl, Br, I, OH, NH2, CN; svaki n i m je neovisno izabran od 0, 1, 2 ili 3, i n i m nisu istovremeno 0; svaki L1 i L2 je neovisno izabran od -CH2-, -CH2CH2-, -O-, -C(=O)- i - C(=O)-NH-; Ra je neovisno izabran od H, F, Cl, Br, I, OH, NH2, CN, C1-3 alkila, C1-3 alkoksi i C1-3 alkilamino, pri čemu, svaki C1-3 alkil, C1-3 alkoksi i C1-3 alkilamino je neovisno i izborno supstituiran sa 1, 2 ili 3 R; Rb je izabran od F, Cl, Br, I, CH3; R je izabran od H, F, Cl, Br, I; svaki heteroaril sa 5 do 6 članova i heterocikloalkil sa 3 do 6 članova neovisno sadrži 1, 2, 3 ili 4 heteroatoma ili grupa heteroatoma neovisno izabranih od -NH-, -O-, -S-, -C(=O)-, -S(=O)- i N.
2. Spoj prikazan kao formula (I) prema patentnom zahtjevu 1, naznačen time što je Ra neovisno izabran od H, F, Cl, Br, I, OH, NH2, CN, CH3, OCH3, NH(CH3) i N(CH3)2.
3. Spoj prikazan kao formula (I) prema patentnom zahtjevu 2, naznačen time što je R2 neovisno izabran od H, C1-3 alkila, C2-4 alkenila i C2-4 alkinila, i, svaki C1-3 alkil, C2-4 alkenil i C2-4 alkinil je neovisno i izborno supstituiran sa 1, 2 ili 3 Ra.
4. Spoj prikazan kao formula (I) prema patentnom zahtjevu 3, naznačen time što je R2 neovisno izabran od H, CH3, vinila i propinila.
5. Spoj prikazan kao formula (I) prema patentnom zahtjevu 1, naznačen time što je M neovisno izabran od ciklopropila, ciklobutila, ciklopentila, cikloheksila, azetidinila, oksetanila, piperidila i morfolinila, i, svaki ciklopropil, ciklobutil, ciklopentil, cikloheksil, azetidinil, oksetanil, piperidil i morfolinil je neovisno i izborno supstituiran sa 1, 2 ili 3 Rb.
6. Spoj prikazan kao formula (I) prema patentnom zahtjevu 5, naznačen time što je M neovisno izabran od piperidila i morfolinila.
7. Spoj prikazan kao formula (I) prema patentnom zahtjevu 1, pri čemu, L1 je izabran od -O- i -C(=O)-NH-; i/ili, L2 je izabran od -C(=O)- i -C(=O)-NH-; i/ili, prsten A je izabran od fenila i piridila.
8. Spoj prikazan kao formula (I) prema patentnom zahtjevu 1, pri čemu je strukturna jedinica [image] izabrana od [image] i [image]
9. Spoj prikazan kao formula (I) prema patentnom zahtjevu 8, pri čemu je strukturna jedinica [image] izabrana od [image] i [image]
10. Spoj prikazan kao formula (I) prema bilo kojem od patentnih zahtjeva 1-7, izabran od: [image] naznačen time što, R1 i R3 su kao što su definirani u patentnom zahtjevu 1; svaki n i m je neovisno izabran od 0, 1, 2 ili 3, i n i m nisu istovremeno 0; R2 je kao što je definiran u bilo kojem od patentnih zahtjeva 1, 3 ili 4; L1 i L2 su kao što su definirani u patentnom zahtjevu 1 ili 7.
11. Spoj prikazan kao formula (I) prema patentnom zahtjevu 10, izabran od: [image] [image] naznačen time što n, m, R1, R2, R3, L1, L2 su kao što su definirani u patentnom zahtjevu 10.
12. Spoj prikazan kao formula (I) prema bilo kojem od patentnih zahtjeva 1-11, izabran od: [image] [image]
13. Spoj prema patentnom zahtjevu 12, izabran od: [image] [image] [image]
14. Farmaceutski pripravak koji sadrži terapeutski efikasnu količinu spoja prema bilo kojem od patentnih zahtjeva 1-13 kao aktivni sastojak, i farmaceutski prihvatljiv nosač.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-13 ili farmaceutski pripravak prema patentnom zahtjevu 14, za uporabu kao lijek srodan BTK inhibitorima; lijek srodan BTK inhibitorima je izborno lijek za liječenje hematološkog tumora i autoimune bolesti; bolest je izborno difuzni B-krupnostanični limfom.
HRP20240283TT 2019-09-26 2020-09-25 Derivati 4-fluoro-1h-pirazolo[3,4-c]piridina kao selektivni inhibitori brutonove tirozin kinaze (btk) za liječenje b-staničnih limfoma i autoimunih bolesti HRP20240283T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201910919180 2019-09-26
CN202010330226 2020-04-24
EP20867917.5A EP4036095B1 (en) 2019-09-26 2020-09-25 4-fluoro-1h-pyrazolo[3,4-c]pyridine derivatives as selective bruton's tyrosine kinase (btk) inhibitors for the treatment of b-cell lymphoma and autoimmune diseases
PCT/CN2020/117690 WO2021057893A1 (zh) 2019-09-26 2020-09-25 作为选择性btk激酶抑制剂的吡唑并吡啶类化合物

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US (1) US11739090B2 (hr)
EP (1) EP4036095B1 (hr)
JP (1) JP7213604B2 (hr)
KR (1) KR102500569B1 (hr)
CN (1) CN114450289B (hr)
AU (1) AU2020355845B2 (hr)
BR (1) BR112022005729A2 (hr)
CA (1) CA3152587C (hr)
DK (1) DK4036095T3 (hr)
FI (1) FI4036095T3 (hr)
HR (1) HRP20240283T1 (hr)
LT (1) LT4036095T (hr)
MX (1) MX2022003707A (hr)
PL (1) PL4036095T3 (hr)
PT (1) PT4036095T (hr)
RS (1) RS65239B1 (hr)
SI (1) SI4036095T1 (hr)
WO (1) WO2021057893A1 (hr)

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KR20230154243A (ko) * 2021-03-23 2023-11-07 점보 드러그 뱅크 컴퍼니 리미티드 불소-치환된 피리도피라졸계 화합물의 결정형 및 이의 제조 방법
WO2024022234A1 (zh) * 2022-07-28 2024-02-01 成都嘉葆药银医药科技有限公司 吡唑并吡啶类化合物在制备治疗包括中枢神经系统疾病的btk相关疾病的药物中的用途

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201508035TA (en) * 2007-03-28 2015-10-29 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
US20150152115A1 (en) * 2007-12-27 2015-06-04 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
KR20120116387A (ko) 2009-08-27 2012-10-22 폴리머스 씨알씨 리미티드 나노 은-산화아연 조성물
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014113942A1 (en) * 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014199171A1 (en) * 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors
EP3082811B1 (en) * 2013-12-20 2020-01-15 Merck Sharp & Dohme Corp. Btk inhibitors
WO2015095099A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Btk inhibitors
CN105017256A (zh) * 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
CN105085474B (zh) * 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN105399756B (zh) 2014-09-05 2019-06-25 广东东阳光药业有限公司 Btk抑制剂及其用途
WO2016106627A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106652A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
TW201718572A (zh) * 2015-06-24 2017-06-01 普林斯匹亞生物製藥公司 酪胺酸激酶抑制劑
CN105753863B (zh) * 2015-09-11 2018-07-31 东莞市真兴贝特医药技术有限公司 氧代二氢咪唑并吡啶类化合物及其应用
US10662187B2 (en) 2016-01-21 2020-05-26 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
CN109071455B (zh) 2016-03-11 2022-08-02 嘉兴和剂药业有限公司 用于调节布鲁顿酪氨酸激酶的化合物及方法
CN109851620B (zh) * 2016-08-17 2020-08-07 深圳市塔吉瑞生物医药有限公司 用于抑制酪氨酸激酶活性的稠合双环类化合物
JOP20190113A1 (ar) 2016-11-18 2019-05-15 Biocad Joint Stock Co مثبطات بروتون تيروزين كيناز
CN106588937B (zh) * 2017-01-16 2018-09-21 东莞市真兴贝特医药技术有限公司 咪唑并吡嗪类化合物及其制备方法和应用
CN110272416A (zh) 2018-03-14 2019-09-24 武汉宇科源医药生物科技有限公司 吡唑并[3,4-c]吡啶-7-胺衍生物及其制备方法和应用

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US11739090B2 (en) 2023-08-29
JP2022542196A (ja) 2022-09-29
CN114450289A (zh) 2022-05-06
US20220324864A1 (en) 2022-10-13
EP4036095B1 (en) 2024-01-31
AU2020355845B2 (en) 2023-04-06
CN114450289B (zh) 2024-01-02
KR20220061262A (ko) 2022-05-12
PT4036095T (pt) 2024-02-19
KR102500569B1 (ko) 2023-02-16
AU2020355845A1 (en) 2022-05-19
FI4036095T3 (fi) 2024-02-14
LT4036095T (lt) 2024-03-25
EP4036095A4 (en) 2022-12-07
BR112022005729A2 (pt) 2022-06-21
WO2021057893A1 (zh) 2021-04-01
RS65239B1 (sr) 2024-03-29
CA3152587C (en) 2023-05-23
SI4036095T1 (sl) 2024-04-30
PL4036095T3 (pl) 2024-04-15
DK4036095T3 (da) 2024-03-04
MX2022003707A (es) 2022-06-23
JP7213604B2 (ja) 2023-01-27
CA3152587A1 (en) 2021-04-01

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